title: Discovery of pyrazolo[1,5-a]pyrimidine-based Pim inhibitors: a template-based approach.
abstract: The synthesis and hit-to-lead SAR development from a pyrazolo[1,5-a]pyrimidine-derived hit 5 to the identification of a series of potent, pan-Pim inhibitors such as 11j are described.
authors.affiliation: Department of Chemical Research, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States. Electronic address: michael.dwyer@merck.com.
authors.forename: Michael P
authors.initials: MP
authors.lastname: Dwyer
authors.forename: Kartik
authors.initials: K
authors.lastname: Keertikar
authors.forename: Kamil
authors.initials: K
authors.lastname: Paruch
authors.forename: Carmen
authors.initials: C
authors.lastname: Alvarez
authors.forename: Marc
authors.initials: M
authors.lastname: Labroli
authors.forename: Cory
authors.initials: C
authors.lastname: Poker
authors.forename: Thierry O
authors.initials: TO
authors.lastname: Fischmann
authors.forename: Rosemary
authors.initials: R
authors.lastname: Mayer-Ezell
authors.forename: Richard
authors.initials: R
authors.lastname: Bond
authors.forename: Yan
authors.initials: Y
authors.lastname: Wang
authors.forename: Rita
authors.initials: R
authors.lastname: Azevedo
authors.forename: Timothy J
authors.initials: TJ
authors.lastname: Guzi
mesh_terms: D006801:Humans; D011485:Protein Binding; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D051573:Proto-Oncogene Proteins c-pim-1 / Q000037:antagonists & inhibitors* / Q000737:chemistry; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D047428:Protein Kinase Inhibitors; D011720:Pyrazoles; D011743:Pyrimidines; D051573:Proto-Oncogene Proteins c-pim-1; C406031:proto-oncogene proteins pim
keywords: Pan–Pim kinase; pyrazolo[1,5-a]pyrimidine